GNE-131 |
| カタログ番号GC31065 |
GNE-131 は、ヒトナトリウムチャネル NaV1.7 の強力かつ選択的な阻害剤であり、IC50 は 3 nM です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1629063-81-5
Sample solution is provided at 25 µL, 10mM.
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GNE-131 is a potent and selective inhibitor of human sodium channel NaV1.7, with an IC50 of 3 nM.
GNE-131 (Compound 13) shows moderate clearance in human liver microsomes and excellent functional activity against human NaV1.7 with an IC50 of 0.003±0.001 μM. GNE-131 shows excellent potency, good in vitro metabolic stability[1].
GNE-131 shows low in vivo clearance in mouse, rat, and dog. GNE-131 also displays excellent efficacy in a transgenic mouse model of induced pain[1].
[1]. Focken T, et al. Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNaV1.7 Inhibitors for the Treatment of Pain. J Med Chem. 2018 Jun 14;61(11):4810-4831.
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)
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